WO2021240547A3 - Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof - Google Patents

Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof Download PDF

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Publication number
WO2021240547A3
WO2021240547A3 PCT/IN2021/050515 IN2021050515W WO2021240547A3 WO 2021240547 A3 WO2021240547 A3 WO 2021240547A3 IN 2021050515 W IN2021050515 W IN 2021050515W WO 2021240547 A3 WO2021240547 A3 WO 2021240547A3
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WO
WIPO (PCT)
Prior art keywords
solid forms
preparation
sphingosine
methods
receptor modulators
Prior art date
Application number
PCT/IN2021/050515
Other languages
French (fr)
Other versions
WO2021240547A2 (en
Inventor
Srinivas Laxminarayan Pathi
Puppala RAVI KUMAR
Ramanaiah CHENNURU
Durga Surya Narayana YARRA
Yellanki JAGANNADHAM
Siva Krishna NANGEDDA
Lakkireddy PULLAREDDY
Raju Barla
Original Assignee
Cipla Limited
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cipla Limited filed Critical Cipla Limited
Priority to EP21740247.8A priority Critical patent/EP4139282A2/en
Priority to US18/000,121 priority patent/US20230212115A1/en
Publication of WO2021240547A2 publication Critical patent/WO2021240547A2/en
Publication of WO2021240547A3 publication Critical patent/WO2021240547A3/en
Priority to ZA2022/12800A priority patent/ZA202212800B/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C207/00—Compounds containing nitroso groups bound to a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/14—Adipic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to process for preparation of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxy imino]ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid, intermediates, salts and solid forms thereof to pharmaceutical compositions comprising the salts and solid forms and to use of said compositions for the treatment of multiple sclerosis, particularly secondary progressive multiple sclerosis.
PCT/IN2021/050515 2020-05-29 2021-05-27 Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof WO2021240547A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP21740247.8A EP4139282A2 (en) 2020-05-29 2021-05-27 Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof
US18/000,121 US20230212115A1 (en) 2020-05-29 2021-05-27 Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forme thereof
ZA2022/12800A ZA202212800B (en) 2020-05-29 2022-11-24 Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN202021022647 2020-05-29
IN202021022647 2020-05-29
IN202021038947 2020-09-09
IN202021038947 2020-09-09
IN202021050037 2020-11-17
IN202021050037 2020-11-17

Publications (2)

Publication Number Publication Date
WO2021240547A2 WO2021240547A2 (en) 2021-12-02
WO2021240547A3 true WO2021240547A3 (en) 2022-01-06

Family

ID=76859683

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2021/050515 WO2021240547A2 (en) 2020-05-29 2021-05-27 Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof

Country Status (4)

Country Link
US (1) US20230212115A1 (en)
EP (1) EP4139282A2 (en)
WO (1) WO2021240547A2 (en)
ZA (1) ZA202212800B (en)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010080409A1 (en) * 2008-12-18 2010-07-15 Novartis Ag Hemifumarate salt of 1- [4- [1- ( 4 -cyclohexyl-3 -trifluoromethyl-benzyloxyimino ) -ethyl] -2 -ethyl-benzyl] -a zetidine-3-carboxylic acid
WO2019064184A1 (en) * 2017-09-27 2019-04-04 Dr. Reddy's Laboratories Limited Process for preparation of siponimod, its salts and solid state forms thereof
WO2019144094A1 (en) * 2018-01-22 2019-07-25 Teva Pharmaceuticals International Gmbh Crystalline siponimod fumaric acid and polymorphs thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
CA2862375A1 (en) 2012-02-03 2013-08-08 Novartis Ag Process for preparing n-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010080409A1 (en) * 2008-12-18 2010-07-15 Novartis Ag Hemifumarate salt of 1- [4- [1- ( 4 -cyclohexyl-3 -trifluoromethyl-benzyloxyimino ) -ethyl] -2 -ethyl-benzyl] -a zetidine-3-carboxylic acid
WO2019064184A1 (en) * 2017-09-27 2019-04-04 Dr. Reddy's Laboratories Limited Process for preparation of siponimod, its salts and solid state forms thereof
WO2019144094A1 (en) * 2018-01-22 2019-07-25 Teva Pharmaceuticals International Gmbh Crystalline siponimod fumaric acid and polymorphs thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MINO R CAIRA ED - MONTCHAMP JEAN-LUC: "CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS", TOPICS IN CURRENT CHEMISTRY; [TOPICS IN CURRENT CHEMISTRY], SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP001156954, ISSN: 0340-1022, [retrieved on 19990226], DOI: 10.1007/3-540-69178-2_5 *

Also Published As

Publication number Publication date
EP4139282A2 (en) 2023-03-01
ZA202212800B (en) 2024-04-24
US20230212115A1 (en) 2023-07-06
WO2021240547A2 (en) 2021-12-02

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